U.S. Pat. No. 4,748,246 discloses substituted pyrazolo [4.3-C] quinolines having the formula: ##STR2## which are disclosed as being able to antagonize the activity of interleukin-1 (IL-1) and as being useful as anti-inflammatory agents in the treatment of disease states involving enzymatic tissue destruction.
European Patent Application, Publication No. 0 120 483A1 published Oct. 3, 1984 (Application No. 84103231.1 filed Mar. 23, 1984) discloses (1H-tetrazol-5-yl)-2(1H)-quinolones of the formula: ##STR3##
In the formula "A" is --CH.dbd. or --N.dbd.; "R" is H or alkyl of 1-4C; "n" is 0, 1 or 2; and "X" is H, alkyl of 1-4C, alkoxy of 1-4C, halogen, methylmercapto, methylsulfonyl, or two X's can be combined as methylenedioxy; with the proviso that, when X is methylmercapto or methylsulfonyl, then n must be 1. The document discloses that the compounds are useful as anti-allergy agents.
European Patent Application, Publication No. 0 226 357A1, published Jun. 24, 1987 (Application No. 86309207.8 filed Nov. 11, 1986) discloses substituted 2-(1H)-quinolones of the formula: ##STR4##
In the formula "Het" is a 5-membered monocyclic aromatic heterocyclic group containing at least one nitrogen atom in the aromatic ring and attached by a nitrogen atom to the 5-, 6-, 7- or 8-position of the quinolone. In the formula "R", which is attached to the 5-, 6-, 7- or 8-position of the quinolone, is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, CF.sub.3, halo, cyano or hydroxymethyl. According to the document, these compounds are cardiac stimulants.
Commonly used non-steroidal anti-inflammatory agents such as aspirin, indomethacin and piroxicam act by inhibiting the cyclooxygenase enzyme, frequently leading to such side effects as gastric irritation and ulcers. Thus, there is a need for compounds with anti-inflammatory properties which do not cause or show a marked reduction in the incidence of such side effects. This invention provides compounds having anti-inflammatory as well as anti-allergy activity which affects both 5-lipoxygenase (5-LO) and cyclooxygenase (CO) derived mediators and should lead to less incidence of serious side effects.